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US 2003/0144325 A1Published application
Isoindolines, method of use, and pharmaceutical compositions
AssigneeCelgene Corporation
InventorsGeorge W. Muller, David I. Stirling, Roger Shen-Chu Chen
Life of this patent
Estimating the term…
Abstract
Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines reduce the levels of TNFα in a mammal. Typical embodiments are 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafuoroisoindoline and 1,3-dioxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4-aminoisoindoline.
Claims8
A 2,6-dioxopiperidine selected from the group consisting of (a) a compound of the formula:
- 7
- in which:
- one of X and Y is C═O and the other of X and Y is C═O or CH2,
- (i) each of R1, R2, R3, and R4, independently of the others, is halo, alkyl of 1 to 4 carbon atoms, or alkoxy of 1 to 4 carbon atoms or (ii) one of R1, R2, R3, and
- R4 is —NHR5 and the remaining of R1, R2, R3, and R4 are hydrogen;
- R5 is hydrogen or alkyl of 1 to 8 carbon atoms;
- R6 is hydrogen, alkyl of 1 to 8 carbon atoms, benzyl, or halo;
- provided that R6 is other than hydrogen if X and Y are C═O and (i) each of R1, R2, R3, and R4 is fluoro or (ii) one of R1, R2, R3, or R4 is amino;
- and
- (b) the acid addition salts of said compounds which contain a nitrogen atom capable of being protonated.
7 more elements
The method of reducing undesirable levels of TNFα in a mammal which comprises administering thereto an effective amount of a compound of the formula
- 8
- in which in said compound one of X and Y is C═O and the other of X and Y is C═O or CH2.
Dependencies are inferred from the claim text.